JP2001278812A - Disintegrant for tablet and tablet using the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a disintegrant capable of easily producing, through ordinary process without complication and at low cost, tablets readily disintegrable at least comparable to those with well-known disintegrants, quickly disintegrable even in the mouth, having sweetness as well because of containing glycine, therefore easily administrable to infants or babies. SOLUTION: This disintegrant comprises glycine. The other objective tablets are obtained by formulating the disintegrant.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a disintegrant for tablets and tablets using the same.

[0002]

2. Description of the Related Art Various techniques have been disclosed or put into practical use as conventional techniques for producing easily disintegrable solid drugs. For example, rapid dissolving technology in the oral cavity (Zydis) developed by R.P.C. Sheila, JP-B-58-24410, "Porous tablets with good disintegration", JP-A-2650493, "Quick-dissolving tablets", and JP-A-2807346. Japanese Patent Application Laid-Open Publication No. 5-27054, "Oral Disintegrating Tablets and Production Method", and the like.

[0003] The production method used in each of the above disclosed techniques is a method in which various compositions are heated and melted, filled and formed, and then cooled and solidified, or after being filled and press-molded in a wet state. It is a method of drying. Recently, a method for producing a fast-dissolving tablet by a method completely different from the above-mentioned method has been disclosed (Japanese Patent No. 2919771). This production method is characterized by comprising a humidifying step for absorbing the pressure-molded tablet and a drying step for drying the humidified tablet.

However, in the techniques disclosed therein,
There is a problem that manufacturing becomes complicated and complicated, and the production cost increases.

[0005]

SUMMARY OF THE INVENTION The present invention has been completed in view of the above circumstances, and has as its object the purpose of making the production not complicated and complicated, the production cost not to be high, and the above-mentioned technology. An object of the present invention is to provide a tablet having a disintegration property equal to or higher than that of a manufactured tablet.

[0006]

The present invention relates to the following tablet disintegrant and tablet.

(1) Disintegrant for tablets containing glycine.

(2) The disintegrant for tablets according to the above (1), further comprising a disintegrant other than glycine and / or a disintegration aid.

(3) A tablet containing the disintegrant according to (1) and an active ingredient.

(4) The tablet according to the above (3), wherein the content of glycine is 20% by weight or more.

(5) The tablet according to the above (3), wherein the content of glycine is 30% by weight or more.

(6) The tablet according to the above (3), further comprising carboxymethyl cellulose and / or corn starch as a disintegrant other than glycine.

[0013]

BEST MODE FOR CARRYING OUT THE INVENTION The disintegrant for tablets of the present invention contains glycine as an essential component. The amount of glycine in the tablet disintegrant is not particularly limited, and can be appropriately set such that the amount of glycine in the tablet containing the tablet disintegrant is 10% by weight to 80% by weight.

When the tablet is to be disintegrated in the stomach and intestine, the amount of glycine in the disintegrant for tablets is set so that the amount of glycine in the tablet is 10% by weight to 20% by weight. It is preferred to do so.

When the tablet is to be disintegrated in the oral cavity, the amount of glycine is set so as to be preferably at least 20% by weight, more preferably at least 30% by weight in the tablet. In particular, when other disintegrating agent or disintegrating agent described below is not used, the amount of glycine is preferably 50% by weight or more. The upper limit of the amount of glycine is 80.
% By weight is preferred. The reason for this is that if the amount of glycine exceeds 80% by weight, tableting failure will occur and the tablet will soften due to moisture absorption at room temperature.

The disintegrant for tablets of the present invention may contain other known disintegrants and / or disintegration aids. Known disintegrants include alginic acid, sodium alginate, pregelatinized starch, sodium carboxymethyl starch, carboxymethylcellulose, carmellose sodium, carmellose potassium, croscarmellose sodium, crospovidone, crystalline cellulose and carmellose sodium, low degree of substitution. Hydroxypropylcellulose (the amount of hydroxypropoxyl group is 5% to 16% according to the method for quantifying low-substituted hydroxypropylcellulose described in the Japanese Pharmacopoeia), dextrin, corn starch, tragacanth powder, potato starch, hydroxypropyl starch, part Alpha-modified starch and the like, especially low-substituted hydroxypropylcellulose, croscarmellose sodium, partially pregelatinized starch, carbohydrate Shi methylcellulose, hydroxypropyl starch, preferably corn starch, and more preferably further carboxymethyl cellulose and corn starch. These disintegrants can be used alone or in combination of two or more.

As disintegration aids, sorbitan fatty acid esters, polysorbate 80, macrogol 1500,
Macrogol 400, Macrogol 4000, Macrogol 6000, sodium lauryl sulfate and the like. By appropriately setting the amount of the other disintegrant and / or disintegration aid to be about 3% by weight to 20% by weight in the tablet, a tablet having excellent disintegration properties can be obtained.

The disintegrant for tablets of the present invention may be in the form of a powder as long as glycine is uniformly incorporated in the tablet composition.
There is no limitation on its form such as granules, and it is produced by a conventional method.

The tablet disintegrant of the present invention is incorporated into a tablet composition by a conventional formulation means and functions as a tablet disintegrant. Tablets containing the tablet disintegrant of the present invention,
It has a disintegration property equal to or higher than that of a tablet containing a known disintegrant such as lactose.

Tablets containing the tablet disintegrant of the present invention include not only pharmaceuticals but also quasi-drugs and tablets taken or eaten as foods. In addition to those intended for the treatment or prevention of, the ingredients contained in quasi-drugs and health foods are also included.

Active ingredients for the treatment and prevention of diseases include antipyretics, analgesics and anti-inflammatory drugs, general cold remedies, gastrointestinal drugs, gastrointestinal function regulators, arrhythmia drugs, antihypertensive drugs, antitussive expectorants, psychotropic drugs, and hypnotics. Examples include sedatives, antihypertensives, dental and oral medicines, and the like. Active ingredients contained in quasi-drugs and health foods include vitamin A, vitamin B ₁ , vitamin B ₂ , nicotinic acid, pantothenic acid, vitamin B ₆ , vitamin B ₁₂ , folic acid, vitamin E, vitamin K, vitamin H And the like, minerals such as iron, magnesium, calcium, and potassium, and dietary fiber.

More specifically, as antipyretics, analgesics and anti-inflammatory drugs, and general cold remedies, acetaminophen, isopropylantipyrine, ibuprofen, etensamide, phenacetin, sulpyrine, aspirin, aminopyrine, antipyrine, indomethacin, phenylbutazone, oxyphene Butazone, mefenamic acid, meperizole and the like are exemplified, and as a gastrointestinal drug, a gastrointestinal function regulator, diastase, Takadiastase, pancreatin, metoclopramide,
Trimebutine maleate, cisapride, sodium bicarbonate, precipitated calcium carbonate, magnesium oxide, synthetic aluminum silicate, propantheline bromide, secretin,
Cimetidine and the like are exemplified.

The tablet of the present invention may further contain a lubricant and a binder. Lubricants include magnesium stearate, calcium stearate, talc, sodium lauryl sulfate, liquid paraffin, and the like. Examples of the binder include starch and hydroxypropylcellulose (the amount of hydroxypropoxyl group according to the method for determining hydroxypropylcellulose described in the Japanese Pharmacopoeia is 53% to 53%).
78%), polyvinylpyrrolidone, polyvinyl alcohol, hydroxypropylmethylcellulose, methylcellulose and the like.

To produce tablets using the tablet disintegrant of the present invention, conventional devices and methods for tablet production are used. Specifically, the disintegrant for tablets of the present invention as an active ingredient,
After adding the appropriate additives such as excipients and mixing them into granules by a method known per se, adding a lubricant and the like,
Compression molding is performed using a rotary tableting machine or the like.

More specifically, an active ingredient, a disintegrating agent for tablets of the present invention, an excipient, and the like are mixed in a kneader and mixed. After mixing, a binder in which a binder is dissolved is dropped, and kneading and granulation is performed. After sufficient kneading, the granules are dried with a dryer and sized with a crusher. Further, after adding and mixing a lubricant and the like, the mixture is compression-molded by a rotary tableting machine.

[0026]

According to the tablet disintegrant of the present invention, easily disintegratable tablets can be easily produced by a conventional tablet production method. Therefore, the production of tablets does not become complicated and complicated, and the production cost does not increase. Moreover, according to the tablet disintegrant of the present invention, a tablet having a disintegration property equal to or higher than that of a known disintegrant can be provided.

Furthermore, since the tablet of the present invention disintegrates quickly even in the mouth and contains glycine, it has a sweet taste and the tablet containing the tablet disintegrant of the present invention is administered to children and infants. Easy to do.

[0028]

EXAMPLES Examples of the disintegrant for tablets and tablets of the present invention and test examples are shown below.

Example 1 Glycine was used as a disintegrant for tablets in an amount equivalent to 180 mg of a tablet weighing 250 mg per tablet.

Example 2 Corn starch was added to the tablet disintegrant of Example 1 in an amount corresponding to 65 mg of a tablet weighing 250 mg per tablet.
The tablet was uniformly prepared to prepare a disintegrant for tablets.

Test Example 1 Using the components shown in Table 1,
One tablet weighing 250 mg was manufactured, and the hardness and disintegration time of the tablet in the oral cavity were measured. These results are summarized in Table 2.

(Manufacturing method) Glycine, lactose and corn starch are placed in a vertical granulator (VG-01, manufactured by Powrex) and mixed for 5 minutes. After mixing
Hydroxypropyl cellulose (trade name: Nisso HPC,
Nippon Soda Co., Ltd., hydroxypropoxyl group 53.4% ~
77.5% content, hereinafter also referred to as HPC. ) Aqueous solution (1
0 w / v%) and knead granulation for 5 minutes. After drying, sieving is performed using a Comil (QS-1975, manufactured by Powrex) equipped with a 1.9 mm punching screen. After sizing, magnesium stearate is added and mixed for 10 minutes with a ribbon mixer. Using a rotary tableting machine (Virgo, manufactured by Kikusui Seisakusho), tablets each having a diameter of 8 mm and weighing 250 mg per tablet are produced.

[0033]

[Table 1]

(Experimental Method) Hardness The hardness of 10 tablets was measured using a Monsanto hardness meter, and the average value was shown in Table 2 as hardness (kg).

2. Disintegration time of the tablet in the oral cavity The time from when the tablet was put in the mouth until the tablet completely disappeared was defined as the oral disintegration time of the tablet. The average time (seconds) was determined from five subjects.

[0036]

[Table 2]

From the results of tablet A and tablet D shown in Table 2, tablet A is a conventional tablet D using lactose as a disintegrant.
It can be seen that the tablet has the same hardness as that of the tablet D and the disintegration property of the tablet is superior to that of the tablet D.

[Test Example 2] Corn starch in Tablet B shown in Table 1 was replaced with croscarmellose sodium (Tablet E), low-substituted hydroxypropylcellulose (trade name: L-HPC, Shin-Etsu Chemical Co., Ltd., hydroxypropoxyl A tablet was produced in the same manner as in Test Example 1 except that the tablet was replaced with carboxymethylcellulose (Tablet G) containing 7.0% to 16.0% of the base. The disintegration time was measured. Table 3 summarizes the results.

[0039]

[Table 3]

From the results of Table B and Table 3, Table B
Indicates that the disintegration properties of the tablets are superior to those of tablets E and F and are equivalent to that of tablet G.

[Test Example 3] Using the components shown in Table 4,
Tablets were manufactured in the same manner as in Test Example 1, and the tablet hardness and the oral disintegration time of the tablets were measured. As a result, the hardness was 4.2.
In kg, the oral disintegration time was 15.3 seconds.

[0042]

[Table 4]

Test Example 4 Tablets were prepared in the same manner as in Table 1 except that glycine in Tablet B shown in Table 1 was replaced with L-lysine hydrochloride (Tablet H), L-proline (Tablet I), and L-serine (Tablet J). Was prepared, and the tablet hardness and the oral disintegration time of the tablet were measured in the same manner as in Test Example 1. Table 5 summarizes the results.

[0044]

[Table 5]

From the results of Table B and Table 5, Table B
Indicates that the disintegration properties of tablets are superior to those of tablets H, I and J.

Example 3 Ascorbic acid, glycine, lactose and corn starch were placed in a vertical granulator (VG-01, manufactured by Powrex) and mixed for 5 minutes. After mixing, an aqueous HPC solution (10 w / v%) was added dropwise, and kneading and granulation was performed for 5 minutes. After drying, sieving was performed using a Comil (QS-1975, manufactured by Powrex) equipped with a 1.9 mm punching screen. After sizing, add magnesium stearate and add 1 with a ribbon mixer.
Mix for 0 minutes. Rotary tableting machine (manufactured by Kikusui Seisakusho,
VIRGO) with a diameter of 8 mm and a tablet weight of 250 m.
g tablets were produced. The formulation of the tablet is shown in Table 6.

When the hardness of the tablet and the disintegration time of the tablet in the oral cavity were measured in the same manner as in Test Example 1, the hardness was 3.8 kg.
The disintegration time in the oral cavity was 40.3 seconds.

[0048]

[Table 6]

Example 4 The procedure of Example 3 was repeated, except that ascorbic acid was changed to ethenzamide, and the diameter was 8 m.
A tablet weighing 250 mg was prepared in m. The formulation of this tablet is shown in Table 7. When the hardness of the tablet and the disintegration time in the oral cavity of the tablet were measured in the same manner as in Test Example 1, the hardness of the tablet was 3.6 kg and the disintegration time in the oral cavity was 25.8 seconds.

[0050]

[Table 7]

 ────────────────────────────────────────────────── ─── Continuation of front page (72) Inventor Yasuo Yoshihashi 2-6-31-301 Okubo, Narashino-shi, Chiba F-term (reference) 4C076 AA36 BB01 DD51B EE33B EE38B FF06

Claims (6)

[Claims] 1. A disintegrant for tablets containing glycine. 2. The disintegrating agent for tablets according to claim 1, wherein a disintegrating agent other than glycine and / or a disintegrating aid is blended. 3. A tablet comprising the disintegrant according to claim 1 and an active ingredient. 4. The tablet according to claim 3, wherein the content of glycine is 20% by weight or more. 5. The tablet according to claim 3, wherein the content of glycine is 30% by weight or more. 6. The tablet according to claim 3, further comprising carboxymethyl cellulose and / or corn starch as a disintegrant other than glycine.